BR122020002802B1 - Liofilizado de um sal de hemissulfato do ácido 5,10-metileno-(6r)-tetra-hidrofólico e produto reconstituído - Google Patents

Liofilizado de um sal de hemissulfato do ácido 5,10-metileno-(6r)-tetra-hidrofólico e produto reconstituído Download PDF

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Publication number
BR122020002802B1
BR122020002802B1 BR122020002802-5A BR122020002802A BR122020002802B1 BR 122020002802 B1 BR122020002802 B1 BR 122020002802B1 BR 122020002802 A BR122020002802 A BR 122020002802A BR 122020002802 B1 BR122020002802 B1 BR 122020002802B1
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BR
Brazil
Prior art keywords
thf
water
hemisulfate salt
salt
lyophilized
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BR122020002802-5A
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English (en)
Portuguese (pt)
Inventor
Rudolf Moser
Viola Groehn
Thomas Egger
Thomas Ammann
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Merck & Cie
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Publication of BR122020002802B1 publication Critical patent/BR122020002802B1/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
    • C07D475/02—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4
    • C07D475/04—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
    • C07D475/12—Heterocyclic compounds containing pteridine ring systems containing pteridine ring systems condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
    • C07D475/12—Heterocyclic compounds containing pteridine ring systems containing pteridine ring systems condensed with carbocyclic rings or ring systems
    • C07D475/14—Benz [g] pteridines, e.g. riboflavin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)
BR122020002802-5A 2013-08-14 2014-08-14 Liofilizado de um sal de hemissulfato do ácido 5,10-metileno-(6r)-tetra-hidrofólico e produto reconstituído BR122020002802B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13004050.4 2013-08-14
EP13004050.4A EP2837631A1 (en) 2013-08-14 2013-08-14 New stable salt of 5,10-methylene-(6R)-tetrahydrofolic acid
PCT/EP2014/067447 WO2015022407A1 (en) 2013-08-14 2014-08-14 Hemisulfate salt of 5,10-methylene-(6r)-tetrahydrofolic acid

Publications (1)

Publication Number Publication Date
BR122020002802B1 true BR122020002802B1 (pt) 2022-11-29

Family

ID=48998397

Family Applications (2)

Application Number Title Priority Date Filing Date
BR122020002802-5A BR122020002802B1 (pt) 2013-08-14 2014-08-14 Liofilizado de um sal de hemissulfato do ácido 5,10-metileno-(6r)-tetra-hidrofólico e produto reconstituído
BR112016002770-1A BR112016002770B1 (pt) 2013-08-14 2014-08-14 Sal de hemissulfato de ácido 5,10-metileno-(6r)-tetra-hidrofólico, sua composição farmacêutica e seu uso

Family Applications After (1)

Application Number Title Priority Date Filing Date
BR112016002770-1A BR112016002770B1 (pt) 2013-08-14 2014-08-14 Sal de hemissulfato de ácido 5,10-metileno-(6r)-tetra-hidrofólico, sua composição farmacêutica e seu uso

Country Status (27)

Country Link
US (4) US20160185787A1 (cg-RX-API-DMAC10.html)
EP (3) EP2837631A1 (cg-RX-API-DMAC10.html)
JP (5) JP6617104B2 (cg-RX-API-DMAC10.html)
KR (2) KR102410373B1 (cg-RX-API-DMAC10.html)
CN (2) CN108096200A (cg-RX-API-DMAC10.html)
AU (2) AU2014307872B2 (cg-RX-API-DMAC10.html)
BR (2) BR122020002802B1 (cg-RX-API-DMAC10.html)
CA (1) CA2921178C (cg-RX-API-DMAC10.html)
CY (2) CY1119694T1 (cg-RX-API-DMAC10.html)
DK (2) DK3033344T3 (cg-RX-API-DMAC10.html)
EA (3) EA202091271A3 (cg-RX-API-DMAC10.html)
ES (2) ES2871483T3 (cg-RX-API-DMAC10.html)
HK (1) HK1256262A1 (cg-RX-API-DMAC10.html)
HR (2) HRP20171895T1 (cg-RX-API-DMAC10.html)
HU (2) HUE054504T2 (cg-RX-API-DMAC10.html)
IL (2) IL244069B (cg-RX-API-DMAC10.html)
LT (2) LT3033344T (cg-RX-API-DMAC10.html)
MX (2) MX360355B (cg-RX-API-DMAC10.html)
NO (1) NO3033344T3 (cg-RX-API-DMAC10.html)
NZ (2) NZ717825A (cg-RX-API-DMAC10.html)
PL (2) PL3033344T3 (cg-RX-API-DMAC10.html)
PT (2) PT3287460T (cg-RX-API-DMAC10.html)
RS (2) RS56910B1 (cg-RX-API-DMAC10.html)
SG (2) SG11201601016PA (cg-RX-API-DMAC10.html)
SI (2) SI3033344T1 (cg-RX-API-DMAC10.html)
WO (1) WO2015022407A1 (cg-RX-API-DMAC10.html)
ZA (1) ZA201509204B (cg-RX-API-DMAC10.html)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2837631A1 (en) * 2013-08-14 2015-02-18 Merck & Cie New stable salt of 5,10-methylene-(6R)-tetrahydrofolic acid
US10059710B2 (en) 2016-02-17 2018-08-28 Merck & Cie Stable formulations of 5,10-methylene-(6R)-tetrahydrofolic acid
EP3446703A1 (en) * 2017-08-24 2019-02-27 Isofol Medical AB 6r]-mthf multiple bolus administration in 5-fluorouracil based chemotherapy
EP3446704A1 (en) * 2017-08-24 2019-02-27 Isofol Medical AB [6r]-mthf - an efficient folate alternative in 5-fluorouracil based chemotherapy
PT3668516T (pt) * 2017-08-16 2021-12-23 Merck Patent Gmbh Liofilizados estáveis que compreendem ácido 5,10-metileno-(6r)-tetra-hidrofólico e um ácido dicarboxílico
MX2020007009A (es) * 2018-01-05 2020-11-11 Isofol Medical Ab Metodos para tratar canceres colorrectales metastasicos y colorrectales.
KR20220152385A (ko) * 2020-03-30 2022-11-15 수미토모 케미칼 컴퍼니 리미티드 적층체
CN119325374A (zh) 2022-06-08 2025-01-17 默克专利股份有限公司 包含5,10-亚甲基-(6r)-四氢叶酸的稳定的冻干物
WO2023237483A1 (en) 2022-06-08 2023-12-14 Merck Patent Gmbh Concentrated solutions comprising 5,10-methylene-(6r)-tetrahydrofolic acid
KR20250022144A (ko) 2022-06-08 2025-02-14 메르크 파텐트 게엠베하 5,10-메틸렌-(6R)-테트라히드로폴산 및 NACl을 포함하는 안정한 약학적 조성물
CN119343131A (zh) 2022-06-08 2025-01-21 默克专利股份有限公司 包含5,10-亚甲基-(6r)-四氢叶酸钠的浓缩溶液
WO2023237484A1 (en) 2022-06-08 2023-12-14 Merck Patent Gmbh Compositions comprising disodium 5,10-methylene-(6r)-tetrahydrofolate

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CH697021A5 (de) 2003-06-26 2008-03-31 Merck Eprova Ag Stabile pharmazeutische Zusammensetzungen von 5, 10-Methylentetrahydrofolat.
WO2007064968A2 (en) 2005-12-02 2007-06-07 Adventrx Pharmaceuticals, Inc. Stable pharmaceutical compositions of 5,10 methylenetetrahydrofolate
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JP6617104B2 (ja) 2019-12-04
JP6735321B2 (ja) 2020-08-05
IL269170B (en) 2020-09-30
EP2837631A1 (en) 2015-02-18
JP2019131579A (ja) 2019-08-08
CN105452250B (zh) 2018-02-27
HK1217018A1 (zh) 2016-12-16
PT3033344T (pt) 2018-01-03
CN105452250A (zh) 2016-03-30
NZ717825A (en) 2019-11-29
KR20160043054A (ko) 2016-04-20
HUE037615T2 (hu) 2018-09-28
HRP20210743T1 (hr) 2021-06-25
US12122783B2 (en) 2024-10-22
MX2016001834A (es) 2016-04-15
KR102439605B1 (ko) 2022-09-05
EA201892729A1 (ru) 2019-04-30
MX360355B (es) 2018-10-30
JP7396960B2 (ja) 2023-12-12
BR112016002770B1 (pt) 2022-12-06
RS56910B1 (sr) 2018-05-31
CN108096200A (zh) 2018-06-01
SG10201801179VA (en) 2018-03-28
ES2654474T3 (es) 2018-02-13
SG11201601016PA (en) 2016-03-30
EP3033344B1 (en) 2017-09-27
HUE054504T2 (hu) 2021-09-28
CY1119694T1 (el) 2018-04-04
DK3287460T3 (da) 2021-05-03
HK1256262A1 (zh) 2019-09-20
EP3287460A1 (en) 2018-02-28
EA201600172A1 (ru) 2016-07-29
IL269170A (en) 2019-11-28
AU2018278943B2 (en) 2019-12-05
NZ745811A (en) 2020-05-29
EP3033344A1 (en) 2016-06-22
NO3033344T3 (cg-RX-API-DMAC10.html) 2018-02-24
PL3033344T3 (pl) 2018-02-28
KR102410373B1 (ko) 2022-06-22
US20220024940A1 (en) 2022-01-27
JP6764501B2 (ja) 2020-09-30
EP3287460B1 (en) 2021-02-24
CA2921178C (en) 2020-12-08
DK3033344T3 (en) 2017-12-18
JP2020128410A (ja) 2020-08-27
LT3287460T (lt) 2021-07-26
ES2871483T3 (es) 2021-10-29
ZA201509204B (en) 2017-04-26
EA032179B1 (ru) 2019-04-30
SI3033344T1 (en) 2018-01-31
JP7710356B2 (ja) 2025-07-18
KR20210038995A (ko) 2021-04-08
HRP20171895T1 (hr) 2018-01-26
CA2921178A1 (en) 2015-02-19
US20190106431A1 (en) 2019-04-11
MX382578B (es) 2025-03-13
IL244069B (en) 2019-09-26
PT3287460T (pt) 2021-05-27
IL244069A0 (en) 2016-04-21
US20240400574A1 (en) 2024-12-05
SI3287460T1 (sl) 2021-08-31
AU2014307872A1 (en) 2016-03-24
US20160185787A1 (en) 2016-06-30
EA202091271A2 (ru) 2020-09-30
JP2022024035A (ja) 2022-02-08
JP2018203763A (ja) 2018-12-27
WO2015022407A1 (en) 2015-02-19
PL3287460T3 (pl) 2021-07-19
JP2016528242A (ja) 2016-09-15
LT3033344T (lt) 2017-12-27
AU2018278943A1 (en) 2019-01-17
AU2014307872B2 (en) 2018-09-27
BR112016002770A2 (pt) 2017-08-01
RS61986B1 (sr) 2021-07-30
EA202091271A3 (ru) 2020-11-30
CY1124076T1 (el) 2022-05-27

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